A Novel Liposomal Dexamethasone Palmitate Formulation and Anti‐inflammatory Effects on Mice

Abstract

A novel dexamethasone palmitate liposomal long-circulating (DPL long-circulating) drug delivery system was established. The DPL long-circulating and DPL (dexamethasone palmitate liposomal) systems were prepared by film-distributed extrusion with phospholipid and cholesterol. The formulation stability of DPL long-circulating and DPL were investigated. The anti-inflammatory activity and acute toxicity of DPL long-circulating, DPL and dexamethasone sodium phosphate injection (DSP) were evaluated with mice. The DPL long-circulating systems were successfully prepared by film-distributed extrusion methods. The experimental results showed that the DPL long-circulating had uniform particle size and stable property. The DPL long-circulating and DPL showed stronger anti-inflammatory effect than DSP in an anti-inflammatory test. Acute toxicity tests showed that DSP injection had lower toxicity than the DPL long-circulating and DPL, which suggested that DPL long-circulating and DPL had higher bioavailability with passive targeting efficacy of liposomes. The DPL long-circulating formulation product can meet quality requirement. This formulation had stronger anti-inflammatory effect and higher acute toxicity.

Glucocorticoids-based prodrug design: Current strategies and research progress

“…This increased solubility allows for higher drug loading in lipid carriers such as nanoparticles or liposomes. On the other hand, lipophilic prodrugs tend to partition preferentially into the lipid phase of the carrier, and this high-affinity property with lipid materials will exhibit slower release kinetics and, therefore, contribute to sustained release and prolonged therapeutic effects [145] . These prodrugs are usually made from aliphatic acids or aliphatic alcohols linked to the drug through different linkers, with aliphatic compounds comprising 16 carbons or 18 carbons being the most common.…”

“… [151] Dex palmitate Palmitic acid /Liposome Esterase/ Hydrolysis-activated Ester Intravenous injection To treat AIA and S180-bearing in mice; Improved encapsulation efficiencies of Dex; Actively targets the disease sites; Enhanced therapeutic effects. [ 12 , 145 , 152 ] Dex palmitate Palmitic acid /Nanoparticle Esterase/ Hydrolysis-activated Ester Intravenous injection To treat CIA in mice; Increased drug accumulation in arthritic joints; Enhanced therapeutic effects; Reduced the side effects. [147] Budesonide palmitate Palmitic acid /Nanoparticle Esterase/ Hydrolysis-activated Ester At cellular level; To treat LPS-induced cell inflammation; Modification of mannitol increases cellular internalization of liposomes; Enhanced anti-inflammatory ability.…”

“…Limethason®, a lipid emulsion injection loaded with DXP, has been available in Japan since 1988 for treating arthritis [146] , [147] , [148] . Encouraged by this, DXP-related drug delivery systems have gained much attention from researchers, such as emulsions [ 149 , 150 ], liposomes [ 12 , 145 , 151 , 152 ], lipid nanoparticles [ 147 , [153] , [154] , [155] , [156] ], and microparticles [157] . Representatively, Daull et al prepared DXP emulsion and preliminarily evaluated its sustained-release effect after intravitreous injection [149] .…”

A Simple and Sensitive Piezoelectric Immunosensor for Cholera Toxin Based on GM1‐Incorporated Liposome Agglutination

“…13,14 Liposomes, spherical vesicles composed of a phospholipid bilayer surrounding an aqueous cavity, were originally developed to study cell membranes. 15 However, because of their ability to carry different agents in the aqueous cavity, liposomes have been utilized in diagnostics, in drug delivery, and even by the cosmetics and food industries. Liposomes used in detection assay systems mostly occur as immunoliposomes with antibodies bound to the surface and also as DNA-or analyte-tagged liposomes.…”